Li Yi-Lun, Shi Zhaojiang, Shen Tao, Ye Ke-Yin
Institute of Pharmaceutical Science and Technology, College of Chemistry, Fuzhou University, Fuzhou 350108, China.
Frontiers Science Center for Transformative Molecules, School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai 200240, China.
Beilstein J Org Chem. 2022 Aug 12;18:1026-1031. doi: 10.3762/bjoc.18.103. eCollection 2022.
α-Azidoketones are valuable and versatile building blocks in the synthesis of various bioactive small molecules. Herein, we describe an environmentally friendly and efficient electrochemical vicinal oxyazidation protocol of α-arylvinyl acetates to afford diverse α-azidoketones in good yields without the use of a stoichiometric amount of chemical oxidant. A range of functionality is shown to be compatible with this transformation, and further applications are demonstrated.
α-叠氮基酮是合成各种生物活性小分子中具有价值且用途广泛的结构单元。在此，我们描述了一种环境友好且高效的电化学邻位氧叠氮化反应方法，该方法可将α-芳基乙烯基乙酸酯转化为多种α-叠氮基酮，产率良好，且无需使用化学计量的化学氧化剂。一系列官能团被证明与该转化反应兼容，并展示了其进一步的应用。
